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Structure-Guided Design and Development of Novel Cyclophilin A Inhibitors and Ganoderiol-F Derivatives: An In-Silico Approach
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Molecular modeling, synthesis, and biological evaluation of macrocyclic calpain inhibitors
Andrew D Abell1, Matthew A Jones, James M Coxon
1Department of Chemistry, University of Canterbury, Private Bag 4800, Christchurch, New Zealand.
Angewandte Chemie (International Ed. in English)
|January 16, 2009
Abstract:
The design and elaboration of a series of macrocyclic templates that exhibit a propensity to adopt a beta-strand-like peptide-backbone conformation led to potent and selective inhibitors of calpain 2. Macrocycle 1 retarded calcium-induced opacification in an ovine-lens culture assay and is a lead compound for the development of a drug for cataract treatment. Cbz=carbobenzyloxy.
